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A pharmaceutical composition comprising a sulfonylurea drug and preparation method thereof

Active Publication Date: 2020-01-23
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a new combination of a sulfonylurea drug (glibenclamide) with a cyclodextrin and an additive that improves the solubility and stability of the drug in water and prevents the adsorption of glibenclamide onto PVC infusion bags. This is an unexpected improvement compared to using either cyclodextrin or additive alone.

Problems solved by technology

Sulfonylurea drugs are mildly acidic, and has poor solubility in water, especially poor solubility at neutral and acidic pH.
If an acidic pH regulator was used to reduce the pH, there may be a risk of drug precipitation.

Method used

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  • A pharmaceutical composition comprising a sulfonylurea drug and preparation method thereof
  • A pharmaceutical composition comprising a sulfonylurea drug and preparation method thereof
  • A pharmaceutical composition comprising a sulfonylurea drug and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

example 1

Preparation of Glibenclamide Injectable Composition

[0101]

FormulaDosageIngredients(g / 100 ml)SpecificationGlibenclamide0.2Concentration of the active ingredient2 mg / mlMeglumine0.1Concentration of the additive0.1%(w / v)Hydroxypropyl-β-5.0Concentration of the cyclodextrin5%cyclodextrin(w / v)WaterAdd to—100 ml

[0102]Preparation method: According to the formula, the additive and the cyclodextrin were dissolved in 50˜70 ml water, into which was added the glibenclamide powder, with stirring to dissolve, obtaining a solution. The above solution was adjusted to pH 7.0 with 0.1 M hydrochloric acid, and added to 100 ml with water, obtaining a glibenclamide injectable composition.

example 2

Preparation of Glibenclamide Injectable Composition

[0103]

Formula:DosageIngredients(g / 100 ml)SpecificationGlibenclamide0.1Concentration of the active ingredient1 mg / mlMeglumine0.1Concentration of the additive 0.1%(w / v)Hydroxypropyl-β-5.0Concentration of the cyclodextrin 5.0%cyclodextrin(w / v)WaterAdd to—100 ml

[0104]In Example 2, the method for preparing the composition was similar to that of Example 1, with a difference in that the solution formulated according to the formula in Example 2 was adjusted to pH 8.0.

example 3

Preparation of Glibenclamide Injectable Composition

[0105]

Formula:DosageIngredients(g / 100 ml)SpecificationGlibenclamide0.01Concentration of the active ingredient0.1 mg / mlMeglumine0.1Concentration of the additive 0.1%(w / v)Hydroxypropyl-β-2.5Concentration of the cyclodextrin 2.5%cyclodextrin(w / v)WaterAdd to—100 ml

[0106]In Example 3, the method for preparing the composition was similar to that of Example 1, with a difference in that the solution formulated according to the formula in Example 3 was adjusted to pH 7.5.

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Abstract

An injectable pharmaceutical composition of a sulfonylurea drug and a preparation method thereof were described. The pharmaceutical composition contains a sulfonylurea drug, a cyclodextrin and an additive.

Description

TECHNICAL FIELD[0001]The present invention relates to the field of pharmaceutical, especially relates to a pharmaceutical composition for injection containing a sulfonylurea drug and the preparation method thereof.BACKGROUND[0002]A Sulfonylurea drug is an insulin secretagogue, which is widely used in the clinical treatment of type II diabetes. Widely used sulfonylurea drugs in clinical practice include glibenclamide (also referred to as gliburide), gliclazide, glipizide, gliquidone, glibornuride, glimepiride, etc. All the hypoglycemic sulfonylurea drugs in the market are oral solid preparations.[0003]Studies in recent years have shown that glibenclamide (Formula 1, also referred to as Glyburide, whose chemical name is 5 -chloro-N-(4-[N-(cyclohexylcarbamoyl)aminosulfonyl]phenethyl)-2-methoxybenzamide) could be used for the prevention of cerebral edema for patients with stroke when administered by intravenous injection (Sheth et.al, Pilot study of intravenous glyburide in patients wit...

Claims

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Application Information

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IPC IPC(8): A61K31/64A61K47/02A61K47/26A61K47/40A61P3/10
CPCA61K47/02A61P3/10A61K47/26A61K9/08A61K31/64A61K47/40A61K9/19A61K9/0019A61K47/6951C08B37/0015
Inventor ZHONG, WUGAO, CHUNSHENGGONG, WEILI, SONGCHEN, HONGYU
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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